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1. 发明申请

WO2009012954A1 NOVEL ESTROGEN RECEPTOR LIGANDS 审中-公开
标题翻译：新颖的雌激素受体配体
公开(公告)号：WO2009012954A1
公开(公告)日：2009-01-29
申请号：PCT/EP2008/005948
申请日：2008-07-21
申请人： KARO BIO AB , APELQVIST, Theresa , LÖFSTEDT, Anton Joakim , NORIN, Thomas Anders Wilson , WENNERSTAL, Mattias , WU, Xiongyu , HAGBERG, Lars
发明人： APELQVIST, Theresa , LÖFSTEDT, Anton Joakim , NORIN, Thomas Anders Wilson , WENNERSTAL, Mattias , WU, Xiongyu , HAGBERG, Lars
IPC分类号： C07C49/747 , C07C69/76 , C07C209/44 , C07C225/22 , C07C233/14 , C07C251/44 , C07C255/47 , C07C311/08 , C07C311/21 , C07D209/44 , C07D231/56 , C07D261/08 , C07D277/24 , C07D277/34 , C07D333/16
CPC分类号： C07C49/747 , C07C45/513 , C07C45/62 , C07C45/63 , C07C45/65 , C07C45/66 , C07C45/673 , C07C45/676 , C07C45/68 , C07C45/69 , C07C45/71 , C07C45/72 , C07C45/78 , C07C49/753 , C07C49/84 , C07C69/63 , C07C225/22 , C07C233/33 , C07C251/44 , C07C255/47 , C07C311/08 , C07C311/21 , C07C2601/02 , C07C2602/22 , C07C2602/30 , C07D207/333 , C07D209/44 , C07D209/94 , C07D231/56 , C07D261/08 , C07D277/24 , C07D277/34 , C07D307/46 , C07D307/52 , C07D333/16 , C07D333/22 , C07D333/38 , C07C49/633
摘要： The invention provides a compound of formula (I) or a pharmaceutically acceptable ester, amide, solvate or salt thereof, including a salt of such an ester or amide, and a solvate of such an ester, amide or salt, wherein W, X, Y, Z, R 1 , R 2 , R 7 , R 8 , R 9 , R 10 , R 11 , R 12 , R 13 , R 14 , R 15 and R 16 are as defined in the specification. The invention also provides also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity.
摘要翻译：本发明提供式（I）化合物或其药学上可接受的酯，酰胺，溶剂合物或其盐，包括这种酯或酰胺的盐，以及这种酯，酰胺或盐的溶剂合物，其中W，X， Y，Z，R 1，R 2，R 7，R 8，R 9，R 10，R 11，R 12，R 13，R 14，R 15和R 16如说明书中所定义。本发明还提供了这样的化合物在治疗或预防与雌激素受体活性相关的疾病或病症相关的病症中的用途。

2. 发明申请

WO2010031852A1 NOVEL ESTROGEN RECEPTOR LIGANDS 审中-公开
标题翻译：新颖的雌激素受体配体
公开(公告)号：WO2010031852A1
公开(公告)日：2010-03-25
申请号：PCT/EP2009/062144
申请日：2009-09-18
申请人： KARO BIO AB , RHÖNNSTAD, Patrik , APELQVIST, Theresa , WENNERSTÅL, Mattias , CHENG, Aiping , GORDON, Sandra
发明人： RHÖNNSTAD, Patrik , APELQVIST, Theresa , WENNERSTÅL, Mattias , CHENG, Aiping , GORDON, Sandra
IPC分类号： C07D209/14 , C07D401/04 , C07D403/04 , C07D407/04 , C07D409/04 , C07D413/04 , A61K31/404 , A61K31/4155 , A61K31/4178 , A61K31/422 , A61P19/08 , A61P19/10 , A61P19/02 , A61P15/12 , A61P9/00
CPC分类号： C07D403/04 , C07D209/14 , C07D405/04 , C07D409/04 , C07D413/04
摘要： The invention provides a compound of formula (I) or a pharmaceutically acceptable ester, amide, solvate or salt thereof, including a salt of such an ester or amide, and a solvate of such an ester, amide or salt. The invention also provides also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity. wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 ,R 9 , R 10 and R 11 are as defined in the specification.
摘要翻译：本发明提供式（I）化合物或其药学上可接受的酯，酰胺，溶剂化物或其盐，包括这种酯或酰胺的盐，以及这种酯，酰胺或盐的溶剂合物。本发明还提供了这样的化合物在治疗或预防与雌激素受体活性相关的疾病或病症相关的病症中的用途。其中R1，R2，R3，R4，R5，R6，R7，R8，R9，R10和R11如说明书中所定义。

3. 发明申请

WO2011042473A2 NOVEL ESTROGEN RECEPTOR LIGANDS 审中-公开
标题翻译：新颖的雌激素受体配体
公开(公告)号：WO2011042473A2
公开(公告)日：2011-04-14
申请号：PCT/EP2010/064939
申请日：2010-10-06
申请人： KARO BIO AB , WENNERSTÅL, Mattias , RHÖNNSTAD, Patrik , CHENG, Aiping , GORDON, Sandra , APELQVIST, Theresa , HAGBERG, Lars
发明人： WENNERSTÅL, Mattias , RHÖNNSTAD, Patrik , CHENG, Aiping , GORDON, Sandra , APELQVIST, Theresa , HAGBERG, Lars
IPC分类号： C07D207/32 , C07D409/04 , C07D413/04 , C07D417/04 , A61K31/404 , A61K31/42 , A61K31/425 , A61P9/00 , A61P19/00 , A61P25/00 , A61P37/00
CPC分类号： C07D207/32 , C07D409/04 , C07D413/04 , C07D417/04
摘要： The invention provides a compound of formula (I) or a pharmaceutically acceptable ester, amide, solvate or salt thereof, including a salt of such an ester or amide, and a solvate of such an ester, amide or salt. The invention also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity. Formula (I) wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 and R 10 are as defined in the specification.
摘要翻译：本发明提供式（I）化合物或其药学上可接受的酯，酰胺，溶剂化物或其盐，包括这种酯或酰胺的盐，以及这种酯，酰胺或盐的溶剂合物。本发明还提供了这样的化合物在治疗或预防与与雌激素受体活性相关的疾病或病症相关的病症中的用途。式（I）其中R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8，R 9和R 10如说明书中所定义。

4. 发明申请

WO2011042474A1 NOVEL ESTROGEN RECEPTOR LIGANDS 审中-公开
标题翻译：新雌激素受体配体
公开(公告)号：WO2011042474A1
公开(公告)日：2011-04-14
申请号：PCT/EP2010/064940
申请日：2010-10-06
申请人： KARO BIO AB , APELQVIST, Theresa , CHENG, Aiping , RHÖNNSTAD, Patrik , HAGBERG, Lars , KRÜGER, Lars
发明人： APELQVIST, Theresa , CHENG, Aiping , RHÖNNSTAD, Patrik , HAGBERG, Lars , KRÜGER, Lars
IPC分类号： C07D471/04 , A61K31/437 , A61P15/12 , A61P19/02 , A61P19/08 , A61P19/10 , A61P9/00 , A61P35/00 , A61P3/00
CPC分类号： C07D471/04
摘要： The invention provides a compound of formula (I) or a pharmaceutically acceptable ester, amide, solvate or salt thereof, including a salt of such an ester or amide, and a solvate of such an ester, amide or salt. The invention also provides also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity. Formula (I) wherein A, B, D, E, R 1 , R 2 , R 6 , R 7 , R 8 and R 9 are as defined in the specification.
摘要翻译：本发明提供式（I）化合物或其药学上可接受的酯，酰胺，溶剂化物或其盐，包括这种酯或酰胺的盐，以及这种酯，酰胺或盐的溶剂合物。本发明还提供了这样的化合物在治疗或预防与与雌激素受体活性相关的疾病或病症相关的病症中的用途。式（I）其中A，B，D，E，R 1，R 2，R 6，R 7，R 8和R 9如说明书中所定义。

5. 发明申请

WO2009127686A1 NOVEL ESTROGEN RECEPTOR LIGANDS 审中-公开
标题翻译：新颖的雌激素受体配体
公开(公告)号：WO2009127686A1
公开(公告)日：2009-10-22
申请号：PCT/EP2009/054521
申请日：2009-04-16
申请人： KARO BIO AB , RHÖNNSTAD, Patrik , KALLIN, Elisabet , APELQVIST, Theresa , WENNERSTÅL, Mattias , CHENG, Aiping
发明人： RHÖNNSTAD, Patrik , KALLIN, Elisabet , APELQVIST, Theresa , WENNERSTÅL, Mattias , CHENG, Aiping
IPC分类号： C07D209/08 , C07D209/12 , C07D209/22 , C07D209/36 , C07D209/42 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D413/04 , C07D413/14 , A61K31/404 , A61P5/24 , A61P3/06 , A61P13/00
CPC分类号： C07D209/42 , C07D209/08 , C07D209/12 , C07D209/22 , C07D209/36 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D413/04 , C07D413/14 , C07D417/04
摘要： The invention provides a compound of formula (I) or a pharmaceutically acceptable ester, amide, carbamate, solvate or salt thereof, including a salt of such an ester, amide or carbamate, and a solvate of such an ester, amide, carbamate or salt. The invention also provides also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity, wherein R 1 , R 2 , R 3 , R 4 , R 5 and R 6 are as defined in the specification.
摘要翻译：本发明提供式（I）化合物或其药学上可接受的酯，酰胺，氨基甲酸酯，溶剂合物或其盐，包括这种酯，酰胺或氨基甲酸酯的盐，以及这种酯，酰胺，氨基甲酸酯或盐的溶剂合物。本发明还提供了这样的化合物在治疗或预防与雌激素受体活性相关的疾病或病症相关的病症中的用途，其中R1，R2，R3，R4，R5和R6如说明书中所定义。

6. 发明授权

EP1165595B1 LIVER SPECIFIC BILE ACID DERIVATIVES OF THE GLUCOCORTICOID ANTAGONIST RU486 有权
标题翻译：糖皮质激素拮抗剂RU486的肝特异性胆汁酸衍生物
公开(公告)号：EP1165595B1
公开(公告)日：2003-05-14
申请号：EP00922530.1
申请日：2000-03-18
申请人： KARO BIO AB
发明人： APELQVIST, Theresa , WU, Jinchang , KOEHLER, Konrad, F.
IPC分类号： C07J41/00 , A61K31/575 , A61P5/46
CPC分类号： C07J41/0061 , C07J41/0083
摘要： Novel glucocorticoid receptor ligands as provided which have general formula (I) in which: R is a hydrogen atom, an aliphatic hydrocarbon, an aromatic hydrocarbon, carboxylic acid or ester thereof, alkenyl carboxylic acid or ester thereof, hydroxy, halogen, or cyano halogen, or cyano, or a pharmaceutically acceptable salt thereof. W is a methine carbon atom (CH) having the R, S, or racemic stereochemistry. X and Z are the same or are different and are a bond, an amide (-CONR'- or -NR'CO-), an amine (-NR'-), and ether (-O-), or a thioether (-S-) and R' is a hydrogen atom, an aliphatic hydrocarbon, or an aromatic hydrocarbon. The subscripts n, o are the same or are different and are integers from one (1) to six (6). m is an integer from zero to 6. Y is hydroxyl group, carboxylic acid or ester thereof, a tetrazole, an acylsulfonamide (-CONHSO2R" or -SO2NHCOR" where R" is an aliphatic or aromatic hydrocarbon), or a pharmaceutically acceptable salt thereof. A method for treating diseases associated with metabolism dysfunction or which are dependent on the expression of a glucocorticoid such as diabetes.
摘要翻译：具有通式（I）的新型糖皮质激素受体配体，其中：R为氢原子，脂族烃，芳族烃，羧酸或其酯，烯基羧酸或其酯，羟基，卤素或氰基卤素或氰基，或其药学上可接受的盐。 W是具有R，S或外消旋立体化学的次甲基碳原子（CH）。 X和Z相同或不同，并且是键，酰胺（-CONR'-或-NR'CO-），胺（-NR'-）和醚（-O-），或硫醚 -S-），R'为氢原子，脂肪族烃或芳香族烃。下标n，o相同或不同，并且是从一（1）到六（6）的整数。 m为0至6的整数.Y为羟基，羧酸或其酯，四唑，酰基磺酰胺（-CONHSO2R“或-SO 2 NHCOR”，其中R“为脂族或芳族烃）或其药学上可接受的盐。治疗与代谢功能障碍有关的疾病或依赖于糖皮质激素例如糖尿病的表达的方法。

7. 发明公开

EP1165595A1 LIVER SPECIFIC BILE ACID DERIVATIVES OF THE GLUCOCORTICOID ANTAGONIST RU486 有权
标题翻译：糖皮质激素拮抗剂RU486的肝特异性胆汁酸衍生物
公开(公告)号：EP1165595A1
公开(公告)日：2002-01-02
申请号：EP00922530.1
申请日：2000-03-18
申请人： KARO BIO AB
发明人： APELQVIST, Theresa , WU, Jinchang , KOEHLER, Konrad, F.
IPC分类号： C07J41/00 , A61K31/575 , A61P5/46
CPC分类号： C07J41/0061 , C07J41/0083
摘要： Novel glucocorticoid receptor ligands as provided which have general formula (I) in which: R is a hydrogen atom, an aliphatic hydrocarbon, an aromatic hydrocarbon, carboxylic acid or ester thereof, alkenyl carboxylic acid or ester thereof, hydroxy, halogen, or cyano halogen, or cyano, or a pharmaceutically acceptable salt thereof. W is a methine carbon atom (CH) having the R, S, or racemic stereochemistry. X and Z are the same or are different and are a bond, an amide (-CONR'- or -NR'CO-), an amine (-NR'-), and ether (-O-), or a thioether (-S-) and R' is a hydrogen atom, an aliphatic hydrocarbon, or an aromatic hydrocarbon. The subscripts n, o are the same or are different and are integers from one (1) to six (6). m is an integer from zero to 6. Y is hydroxyl group, carboxylic acid or ester thereof, a tetrazole, an acylsulfonamide (-CONHSO2R' or -SO2NHCOR' where R' is an aliphatic or aromatic hydrocarbon), or a pharmaceutically acceptable salt thereof. A method for treating diseases associated with metabolism dysfunction or which are dependent on the expression of a glucocorticoid such as diabetes.
摘要翻译：具有通式（I）的新型糖皮质激素受体配体，其中：R为氢原子，脂族烃，芳族烃，羧酸或其酯，烯基羧酸或其酯，羟基，卤素或氰基卤素或氰基，或其药学上可接受的盐。 W是具有R，S或外消旋立体化学的次甲基碳原子（CH）。 X和Z相同或不同，并且是键，酰胺（-CONR'-或-NR'CO-），胺（-NR'-）和醚（-O-），或硫醚 -S-），R'为氢原子，脂肪族烃或芳香族烃。下标n，o相同或不同，并且是从一（1）到六（6）的整数。 m是0至6的整数.Y是羟基，羧酸或其酯，四唑，酰基磺酰胺（-CONHSO2R'或-SO 2 NHCOR'，其中R'是脂族或芳族烃），或其药学上可接受的盐。一种治疗与代谢功能障碍有关的疾病或依赖于糖皮质激素例如糖尿病的表达的方法。

8. 发明公开

EP2176209A1 NOVEL ESTROGEN RECEPTOR LIGANDS 审中-公开
标题翻译： NEUE LIGANDENFÜRDENÖSTROGENREZEPTOR
公开(公告)号：EP2176209A1
公开(公告)日：2010-04-21
申请号：EP08774033.8
申请日：2008-07-21
申请人： KARO BIO AB
发明人： APELQVIST, Theresa , LÖFSTEDT, Anton Joakim , NORIN, Thomas Anders Wilson , WENNERSTAL, Mattias , WU, Xiongyu , HAGBERG, Lars
IPC分类号： C07C49/747 , C07C69/76 , C07C209/44 , C07C225/22 , C07C233/14 , C07C251/44 , C07C255/47 , C07C311/08 , C07C311/21 , C07D209/44 , C07D231/56 , C07D261/08 , C07D277/24 , C07D277/34 , C07D333/16
CPC分类号： C07C49/747 , C07C45/513 , C07C45/62 , C07C45/63 , C07C45/65 , C07C45/66 , C07C45/673 , C07C45/676 , C07C45/68 , C07C45/69 , C07C45/71 , C07C45/72 , C07C45/78 , C07C49/753 , C07C49/84 , C07C69/63 , C07C225/22 , C07C233/33 , C07C251/44 , C07C255/47 , C07C311/08 , C07C311/21 , C07C2601/02 , C07C2602/22 , C07C2602/30 , C07D207/333 , C07D209/44 , C07D209/94 , C07D231/56 , C07D261/08 , C07D277/24 , C07D277/34 , C07D307/46 , C07D307/52 , C07D333/16 , C07D333/22 , C07D333/38 , C07C49/633
摘要： The invention provides a compound of formula (I) or a pharmaceutically acceptable ester, amide, solvate or salt thereof, including a salt of such an ester or amide, and a solvate of such an ester, amide or salt, wherein W, X, Y, Z, R1, R2, R7, R8, R9, R10, R11, R12, R13, R14, R15 and R16 are as defined in the specification. The invention also provides also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity.
摘要翻译：本发明提供式（I）化合物或其药学上可接受的酯，酰胺，溶剂化物或其盐，包括这种酯或酰胺的盐，以及这种酯，酰胺或盐的溶剂合物，其中W，X， Y，Z，R 1，R 2，R 7，R 8，R 9，R 10，R 11，R 12，R 13，R 14，R 15和R 16如说明书中所定义。本发明还提供了这样的化合物在治疗或预防与与雌激素受体活性相关的疾病或病症相关的病症中的用途。

9. 发明授权

EP2276732B1 NOVEL ESTROGEN RECEPTOR LIGANDS 有权
标题翻译：新的配基对雌激素受体
公开(公告)号：EP2276732B1
公开(公告)日：2015-05-20
申请号：EP09731606.1
申请日：2009-04-16
申请人： KARO BIO AB
发明人： RHÖNNSTAD, Patrik , KALLIN, Elisabet , APELQVIST, Theresa , WENNERSTÅL, Mattias , CHENG, Aiping
IPC分类号： C07D209/08 , C07D209/12 , C07D209/22 , C07D209/36 , C07D209/42 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D413/04 , C07D413/14 , A61K31/404 , A61P5/24 , A61P3/06 , A61P13/00
CPC分类号： C07D209/42 , C07D209/08 , C07D209/12 , C07D209/22 , C07D209/36 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D413/04 , C07D413/14 , C07D417/04

10. 发明公开

EP1143948A3 LIVER-SELECTIVE GLUCOCORTICOID ANTAGONIST FOR TREATING DIABETES 审中-公开
标题翻译： LEBERSPEZISCHER糖皮质激素拮抗剂治疗糖尿病
公开(公告)号：EP1143948A3
公开(公告)日：2002-09-11
申请号：EP99925232.3
申请日：1999-06-07
申请人： KARO BIO AB
发明人： APELQVIST, Theresa , EFENDIC, Suad
IPC分类号： A61K31/00
CPC分类号： A61K31/00

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